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Eperezolid

Catalog No.GC16781

Oxazolidinone antibacterial agent

Products are for research use only. Not for human use. We do not sell to patients.

Eperezolid Chemical Structure

Cas No.: 165800-04-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$322.00
In stock
5mg
$293.00
In stock
10mg
$419.00
In stock
50mg
$1,256.00
In stock
100mg
$1,758.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

MIC50: 0.5, 1.0, 2.0, 1.0, 16.0 and 2.0 mg/L for Pcptostreptococcus, Propionibacterium acnes, Ciostridium pefringens, Clostridium dijiicile, Bactrroidesjagilis, and Fusobacterium, respectivley

Anaerobic bacteria are a common cause of serious infections. Anaerobic species which predominate in clinical infections include the Bacteroides fragilis group, Clostridium spp. and Peptostreptococcus spp. The oxazolidinones are a novel class of synthetic antimicrobials inhibiting the initiation of protein synthesis. Two compounds of this class, eperezolid and linezolid have been shown to inhibit Enterococcus faecalis and Enterococcus faecium.

In vitro: Ninety per cent of all tested Propionibacterium acnes (30 strains), PeptostreptococccuJ spp. (50 strains), C. perjringens (50 strains) and C. dficile (50 strains) were inhibited by

In vivo: The in vivo effectiveness of eperezolid and linezolid against one strain each of Enterococcus faecalis and vancomycin-resistant Enterococcus faecium was examined in a rat intraabdominal abscess model. Eperezolid was ineffective at doses of 25 mg/kg of body weight twice daily for the reductions in abscess bacterial density for E. faecalis. Against E. faecium infections, intravenous eperezolid was effective, reducing densities approximately 2 log10 CFU/g [2].

Clinical trials: Oral administration of eperezolid (1 000 mg PO) to healthy volunteers has earlier been reported to yield peak serum concentration of 6.28 mg/L, respectively, while the trough concentration was estimated to be 1.62 mg/L, respectively [3].

References:
[1] Edlund C, Oh H, Nord CE.  In vitro activity of linezolid and eperezolid against anaerobic bacteria. Clin Microbiol Infect. 1999;5(1):51-53.
[2] Schülin T, Thauvin-Eliopoulos C, Moellering RC Jr, Eliopoulos GM.  Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother. 1999;43(12):2873-6.
[3] Schaadt RD, Batts DH, Daley-Yates PT, Pawsey SD, Stalker DJ, Zurenko GE.   Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid. Diagn Microbiol Infect Dis. 1997;28(4):201-4.

Chemical Properties

Cas No. 165800-04-4 SDF
Chemical Name N-[[(5S)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
Canonical SMILES CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCN(CC3)C(=O)CO)F
Formula C18H23FN4O5 M.Wt 394.4
Solubility ≥ 14.05mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5355 mL 12.6775 mL 25.355 mL
5 mM 0.5071 mL 2.5355 mL 5.071 mL
10 mM 0.2535 mL 1.2677 mL 2.5355 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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